JP2014502980A - 勃起不全治療用のピラゾロピリミドン化合物 - Google Patents

勃起不全治療用のピラゾロピリミドン化合物 Download PDF

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Publication number: JP2014502980A
Authority: JP; Japan
Prior art keywords: group; methyl; propyl; phenyl; ethoxy
Prior art date: 2011-01-21
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Pending

Application number

JP2013549708A

Other languages

English (en)

Japanese (ja)

Inventor

ジェンピーンワーン，

ジェングオワーン，

Original Assignee

ジョーアジアーンダードーアファーマスーティカルグループカンパニーリミテッド

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2011-01-21

Filing date

2012-01-20

Publication date

2014-02-06

2012-01-20 Application filed by ジョーアジアーンダードーアファーマスーティカルグループカンパニーリミテッド filed Critical ジョーアジアーンダードーアファーマスーティカルグループカンパニーリミテッド

2014-02-06 Publication of JP2014502980A publication Critical patent/JP2014502980A/ja

Status Pending legal-status Critical Current

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RNFNDJAIBTYOQL-UHFFFAOYSA-N chloral hydrate Chemical compound OC(O)C(Cl)(Cl)Cl RNFNDJAIBTYOQL-UHFFFAOYSA-N 0.000 description 2
229960002327 chloral hydrate Drugs 0.000 description 2
229940117229 cialis Drugs 0.000 description 2
238000001816 cooling Methods 0.000 description 2
239000001767 crosslinked sodium carboxy methyl cellulose Substances 0.000 description 2
235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 2
235000019425 dextrin Nutrition 0.000 description 2
FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 description 2
201000010099 disease Diseases 0.000 description 2
239000007884 disintegrant Substances 0.000 description 2
208000035475 disorder Diseases 0.000 description 2
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238000001035 drying Methods 0.000 description 2
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239000000706 filtrate Substances 0.000 description 2
238000001914 filtration Methods 0.000 description 2
238000011010 flushing procedure Methods 0.000 description 2
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239000008172 hydrogenated vegetable oil Substances 0.000 description 2
239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 2
235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 2
229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 2
UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 2
230000002401 inhibitory effect Effects 0.000 description 2
239000007928 intraperitoneal injection Substances 0.000 description 2
210000003734 kidney Anatomy 0.000 description 2
229940097443 levitra Drugs 0.000 description 2
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229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 description 2
210000004072 lung Anatomy 0.000 description 2
229910052943 magnesium sulfate Inorganic materials 0.000 description 2
235000019341 magnesium sulphate Nutrition 0.000 description 2
239000000594 mannitol Substances 0.000 description 2
235000010355 mannitol Nutrition 0.000 description 2
229920000609 methyl cellulose Polymers 0.000 description 2
239000001923 methylcellulose Substances 0.000 description 2
235000010981 methylcellulose Nutrition 0.000 description 2
230000008693 nausea Effects 0.000 description 2
210000000056 organ Anatomy 0.000 description 2
229940049954 penicillin Drugs 0.000 description 2
210000003899 penis Anatomy 0.000 description 2
230000000144 pharmacologic effect Effects 0.000 description 2
CYQAYERJWZKYML-UHFFFAOYSA-N phosphorus pentasulfide Chemical compound S1P(S2)(=S)SP3(=S)SP1(=S)SP2(=S)S3 CYQAYERJWZKYML-UHFFFAOYSA-N 0.000 description 2
230000035479 physiological effects, processes and functions Effects 0.000 description 2
230000008288 physiological mechanism Effects 0.000 description 2
229920001223 polyethylene glycol Polymers 0.000 description 2
239000013641 positive control Substances 0.000 description 2
239000000843 powder Substances 0.000 description 2
229960003387 progesterone Drugs 0.000 description 2
239000000186 progesterone Substances 0.000 description 2
WAJNANMQOPCIPO-UHFFFAOYSA-N pyrazolo[4,3-d]pyrimidin-7-one Chemical compound O=C1N=CN=C2C=NN=C12 WAJNANMQOPCIPO-UHFFFAOYSA-N 0.000 description 2
239000000376 reactant Substances 0.000 description 2
230000001105 regulatory effect Effects 0.000 description 2
239000000741 silica gel Substances 0.000 description 2
229910002027 silica gel Inorganic materials 0.000 description 2
239000002002 slurry Substances 0.000 description 2
229910052708 sodium Inorganic materials 0.000 description 2
HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical class O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 2
238000013222 sprague-dawley male rat Methods 0.000 description 2
239000005720 sucrose Substances 0.000 description 2
238000006277 sulfonation reaction Methods 0.000 description 2
208000024891 symptom Diseases 0.000 description 2
210000001519 tissue Anatomy 0.000 description 2
231100000419 toxicity Toxicity 0.000 description 2
230000001988 toxicity Effects 0.000 description 2
229940094720 viagra Drugs 0.000 description 2
208000029257 vision disease Diseases 0.000 description 2
230000004393 visual impairment Effects 0.000 description 2
FYADHXFMURLYQI-UHFFFAOYSA-N 1,2,4-triazine Chemical compound C1=CN=NC=N1 FYADHXFMURLYQI-UHFFFAOYSA-N 0.000 description 1
IWDBQZUJYMEUCF-UHFFFAOYSA-N 2-(2-ethoxyphenyl)-5-methyl-7-propyl-1h-imidazo[5,1-f][1,2,4]triazine-4-thione Chemical compound CCCC1=NC(C)=C(C(N2)=S)N1N=C2C1=CC=CC=C1OCC IWDBQZUJYMEUCF-UHFFFAOYSA-N 0.000 description 1
APGNKBSMWFABBD-UHFFFAOYSA-N 2-methyl-7-propyl-1h-imidazo[5,1-f][1,2,4]triazin-4-one Chemical compound N1C(C)=NC(=O)C=2N1C(CCC)=NC=2 APGNKBSMWFABBD-UHFFFAOYSA-N 0.000 description 1
TUBOOZSGASWZDM-UHFFFAOYSA-N 5-(2-ethoxyphenyl)-1-methyl-3-propyl-4h-pyrazolo[4,3-d]pyrimidine-7-thione Chemical compound CCCC1=NN(C)C(C(N2)=S)=C1N=C2C1=CC=CC=C1OCC TUBOOZSGASWZDM-UHFFFAOYSA-N 0.000 description 1
TVEXGJYMHHTVKP-UHFFFAOYSA-N 6-oxabicyclo[3.2.1]oct-3-en-7-one Chemical compound C1C2C(=O)OC1C=CC2 TVEXGJYMHHTVKP-UHFFFAOYSA-N 0.000 description 1
241001061127 Thione Species 0.000 description 1
125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 1
125000000217 alkyl group Chemical group 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Life Sciences & Earth Sciences (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Animal Behavior & Ethology (AREA)
Pharmacology & Pharmacy (AREA)
Biophysics (AREA)
Molecular Biology (AREA)
Epidemiology (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Gynecology & Obstetrics (AREA)
Endocrinology (AREA)
Reproductive Health (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

JP2013549708A 2011-01-21 2012-01-20 勃起不全治療用のピラゾロピリミドン化合物 Pending JP2014502980A (ja)

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CN201110023784.6		2011-01-21
CN2011100237846A CN102134242B (zh)	2011-01-21	2011-01-21	一种用于治疗阳痿的快速长效的化合物
PCT/CN2012/070636 WO2012097750A1 (zh)	2011-01-21	2012-01-20	用于治疗阳痿的吡唑并嘧啶酮化合物和咪唑并三嗪酮化合物

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US (1)	US9221825B2 (ru)
EP (1)	EP2666776A4 (ru)
JP (1)	JP2014502980A (ru)
CN (1)	CN102134242B (ru)
CA (1)	CA2825308C (ru)
RU (1)	RU2555364C2 (ru)
WO (1)	WO2012097750A1 (ru)

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AU2018274599B9 (en) *	2017-05-22	2022-04-07	Topadur Pharma Ag	Novel dual mode of action soluble guanylate cyclase activators and phosphodiesterase inhibitors and uses thereof
CN113493459B (zh) *	2020-04-07	2022-12-13	广州白云山医药集团股份有限公司白云山制药总厂	Pde5抑制剂化合物及其制备方法和应用
PE20240248A1 (es)	2020-12-11	2024-02-19	Ildong Pharmaceutical Co Ltd	Nuevos compuestos como inhibidor dual del receptor de androgenos y de la fosfodiesterasa

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2011
- 2011-01-21 CN CN2011100237846A patent/CN102134242B/zh active Active
2012
- 2012-01-20 CA CA2825308A patent/CA2825308C/en active Active
- 2012-01-20 JP JP2013549708A patent/JP2014502980A/ja active Pending
- 2012-01-20 RU RU2013138731/04A patent/RU2555364C2/ru active
- 2012-01-20 WO PCT/CN2012/070636 patent/WO2012097750A1/zh active Application Filing
- 2012-01-20 US US13/980,736 patent/US9221825B2/en not_active Expired - Fee Related
- 2012-01-20 EP EP12736699.5A patent/EP2666776A4/en not_active Withdrawn

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US20140018351A1 (en)	2014-01-16
CN102134242A (zh)	2011-07-27
RU2555364C2 (ru)	2015-07-10
CA2825308A1 (en)	2012-07-26
CN102134242B (zh)	2013-08-28
US9221825B2 (en)	2015-12-29
EP2666776A1 (en)	2013-11-27
WO2012097750A1 (zh)	2012-07-26
RU2013138731A (ru)	2015-02-27
EP2666776A4 (en)	2014-06-18
CA2825308C (en)	2014-09-16

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